Discovery of a new class of protein farnesyltransferase inhibitors in the arylthiophene series
Screening of the ICSN chemical library led to the discovery of 3-(4-chlorophenyl)-4-cyano-5-thioalkylthiophene 2-carboxylic acids as potent farnesyltransferase inhibitors. Enzymatic kinetic studies showed that this original FTI series belongs to the CaaX
Syntheses and Reactions of 2-Halo-5-thiazolecarboxylates
A variety of 2-halo-5-thiazolecarboxylates was prepared from substituted-3-aminoacrylates and 3-ketoesters.Selective reduction of 2-chloro-5-thiazolecarboxylates 4a, 4i and 4j with sodium borohydride in ethanol provided the corresponding 2-halo-5-thiazolemethanols 27 - 29.Nucleophilic displacement on methyl methanesulfonate (32c) occured selectivity at the 5-substituent to provide 2-chloro-4-(trifluoromethyl)-5-(heteroatom-substituted methyl)thiazoles 32d-f.
Lee, Len F.,Schleppnik, Francis M.,Howe, Robert K.
p. 1621 - 1630
(2007/10/02)
2-Amino-4-substituted-thiazolecarboxylic acids and their derivatives
2-Amino-4-substituted-5-thiazolecarboxylic acids and derivatives thereof, are intermediates for the preparation of 2-substituted-4-substituted-5-thiazolecarboxylic acid derivatives which are herbicidal safeners.
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(2008/06/13)
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